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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
Antihypertensive Drugs: Vasodilators01:23

Antihypertensive Drugs: Vasodilators

Vasodilators, primarily affecting the smooth muscles within arterial and venous walls, are commonly used for hypertension treatment. Medications such as minoxidil and hydralazine primarily target arteries and arterioles, while sodium nitroprusside acts on arterioles and venules. Minoxidil, functioning as a prodrug, is metabolized by hepatic sulfotransferase into its active form, minoxidil sulfate, after oral administration. This metabolite binds to the sulfonylurea receptor (SUR) component of...

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Related Experiment Videos

PDE5 inhibitors and their applications.

M P Giovannoni1, C Vergelli, A Graziano

  • 1Dipartimento di Scienze Farmaceutiche, Università di Firenze, via Ugo Schiff 6, 50019 Sesto Fiorentino Firenze, Italy. mariapaola.giovannoni@unifi.it

Current Medicinal Chemistry
|May 25, 2010
PubMed
Summary

Phosphodiesterase type 5 (PDE5) inhibitors are used for erectile dysfunction and are being investigated for other conditions like pulmonary arterial hypertension. This review covers current and emerging PDE5 inhibitor therapies.

Related Experiment Videos

Area of Science:

  • Enzymology
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Phosphodiesterase type 5 (PDE5) is an enzyme crucial for regulating cyclic nucleotide signaling.
  • PDE5's role in physiological and pathological processes makes it a therapeutic target.
  • Current PDE5 inhibitors are primarily used for erectile dysfunction.

Purpose of the Study:

  • To review PDE5 inhibitors currently in clinical use.
  • To analyze PDE5 inhibitors undergoing clinical trials for various conditions.
  • To discuss representative chemical classes of PDE5 inhibitors from the last decade.

Main Methods:

  • Literature review of clinical studies.
  • Analysis of drugs in clinical trials.
  • Survey of chemical classes of PDE5 inhibitors.

Main Results:

  • PDE5 inhibitors are established treatments for erectile dysfunction.
  • Several PDE5 inhibitors are in clinical trials for pulmonary arterial hypertension, benign prostatic hyperplasia, and other conditions.
  • Diverse chemical scaffolds targeting PDE5 have been developed.

Conclusions:

  • Selective PDE5 inhibitors offer therapeutic potential beyond erectile dysfunction.
  • Ongoing research is expanding the clinical applications of PDE5 inhibitors.
  • The development of novel PDE5 inhibitor chemical classes continues to be an active area of research.